α-NETA |
Catalog No.GC45213
One-Click Copy Product Info
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α-NETA is a non-competitive inhibitor of choline acetyltransferase (ChAT; IC50=9μM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 115066-04-1
Sample solution is provided at 25 µL, 10mM.
α-NETA is a non-competitive inhibitor of choline acetyltransferase (ChAT; IC50=9μM). α-NETA inhibits ALDH1A1 (IC50=0.04μM) and antagonizes the activity of chemokine-like receptor 1 (CMKLR1), cholinesterase (ChE; IC50=84μM), and acetylcholinesterase (AChE; IC50=300μM). α-NETA can be used in research related to cancer and diabetic nephropathy[1-4].
In vitro, α-NETA (5μM) pretreated human gastric cancer AGS cells for 16-24 hours. α-NETA inhibited Chemerin-induced cell migration and invasion and suppressed cell morphological transformation[5]. α-NETA (3μM) treated chemerin-overexpressing human trophoblast cells (HTR8/SVneo) for 24-48 hours. α-NETA induced cell membrane rupture, cytoplasmic leakage, and activated the GSDMD/caspase-4-mediated pyroptosis pathway by increasing the expression of caspase-4 and GSDMD and the secretion of IL-18[6].
In vivo, α-NETA (30mg/kg; once daily) was administered by gavage to high-fat diet-induced obese C57BL/6 mice for 4 weeks. α-NETA reduced body weight in the mice[7]. α-NETA (10mg/kg; three times per week) was administered via intraperitoneal injection to nude mice bearing UOK101 cell xenograft tumors and SCID mice bearing human ccRCC PDX (UTSW-XP296) models (subcutaneous and orthotopic implantation) for 70 days. α-NETA significantly inhibited tumor growth and reduced lipid deposition within the tumors, while no significant changes in animal health status were observed[8].
References:
[1] Sastry BV, Jaiswal N, Janson V, et al. Relationships between chemical structure and inhibition of choline acetyltransferase by 2-(alpha-naphthoyl)ethyltrimethylammonium and related compounds. Pharmacol Res Commun. 1988 Sep;20(9):751-71.
[2] Graham KL, Zhang JV, Lewén S, et al. A novel CMKLR1 small molecule antagonist suppresses CNS autoimmune inflammatory disease. PLoS One. 2014 Dec 1;9(12):e112925.
[3] Qiao L, Wu X, Zhang J, et al. α-NETA induces pyroptosis of epithelial ovarian cancer cells through the GSDMD/caspase-4 pathway. FASEB J. 2019 Nov;33(11):12760-12767.
[4] Aleksandrov AA, Polyakova NV, Vinogradova EP, et al. The TAAR5 agonist α-NETA causes dyskinesia in mice. Neurosci Lett. 2019 Jun 21;704:208-211.
[5] Kumar JD, Aolymat I, Tiszlavicz L, et al. Chemerin acts via CMKLR1 and GPR1 to stimulate migration and invasion of gastric cancer cells: putative role of decreased TIMP-1 and TIMP-2. Oncotarget. 2019 Jan 4;10(2):98-112.
[6] Tan L, Chen Z, Sun F, et al. Placental trophoblast-specific overexpression of chemerin induces preeclampsia-like symptoms. Clin Sci (Lond). 2022 Feb 25;136(4):257-272.
[7] Zheng C, Zheng Y, Chen X, et al. α-NETA down-regulates CMKLR1 mRNA expression in ileum and prevents body weight gains collaborating with ERK inhibitor PD98059 in turn to alleviate hepatic steatosis in HFD-induced obese mice but no impact on ileal mucosal integrity and steatohepatitis progression. BMC Endocr Disord. 2023 Jan 10;23(1):9.
[8] Wang D, Mahmud I, Thakur VS, et al. GPR1 and CMKLR1 Control Lipid Metabolism to Support the Development of Clear Cell Renal Cell Carcinoma. Cancer Res. 2024 Jul 2;84(13):2141-2154.
| Cell experiment [1]: | |
Cell lines | HTR8/SVneo cells (immortalized human trophoblast cells) |
Preparation Method | HTR8/SVneo cells were maintained in DMEM/F12 medium supplemented with 10% fetal bovine serum (FBS) at 37°C with 5% CO₂. Cells were infected with LV-hChemerin-GFP lentivirus to overexpress chemerin, selected with puromycin, and subsequently exposed to either 1% DMSO (vehicle control) or 3μM α-NETA dissolved in DMSO. |
Reaction Conditions | 3μM; 24-48h |
Applications | α-NETA prevented the inhibitory effects of chemerin overexpression on cell migration, invasion, and tube formation in co-culture with human umbilical vein endothelial cells (HUVECs). |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice (male, 8-10 weeks old) |
Preparation Method | Mice were fed a high-fat diet (HFD, 40 kcal% fat, 2% fructose) for 12 weeks to induce obesity. Then, mice in the α-NETA group received daily treatments of α-NETA (30mg/kg) via gavage for 4 weeks. Mice in the α-NETA+PD group received daily treatment of α-NETA plus PD98059 (0.3mg/kg via tail vein injection). At the end of intervention, mice were sacrificed for analysis of body weight, liver histology, ileal CMKLR1 mRNA, and serum parameters. |
Dosage form | 30mg/kg; daily gavage; for 4 weeks |
Applications | α-NETA reduced body weight gain in HFD-induced obese mice. Combined with PD98059, α-NETA further reduced body weight and alleviated hepatic steatosis. α-NETA down-regulated CMKLR1 mRNA expression in ileum. No impact on ileal ZO-1 or pERK protein expression, and no significant changes in serum endotoxin levels. |
References: | |
| Cas No. | 115066-04-1 | SDF | |
| Canonical SMILES | O=C(CC[N+](C)(C)C)C1=CC2=CC=CC=C2C=C1.[I-] | ||
| Formula | C16H20NO•I | M.Wt | 369.2 |
| Solubility | DMSO: 3mg/ml,Methanol: Soluble | Storage | Store at -20°C, protect from light, stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7086 mL | 13.5428 mL | 27.0856 mL |
| 5 mM | 541.7 μL | 2.7086 mL | 5.4171 mL |
| 10 mM | 270.9 μL | 1.3543 mL | 2.7086 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)